Granular formulation containing cefixime liposomes and preparation method thereof

A technology of cefixime and liposome, which is applied in the field of medicine, can solve the problems of poor solubility, stability and bioavailability, and achieve the effects of improving bioavailability, storage stability, and significant improvement

Inactive Publication Date: 2011-02-09
王丽燕
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Chinese patents CN101606913A and CN101401810A disclose cefixime dispersible tablets and their preparation methods. The dispersible tablets are all made from cefixime raw materials without any modification. The solubility, stability and biological Utilization is poor

Method used

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  • Granular formulation containing cefixime liposomes and preparation method thereof
  • Granular formulation containing cefixime liposomes and preparation method thereof
  • Granular formulation containing cefixime liposomes and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Example 1: Preparation of Cefixime Liposome

[0071] Name of raw materials

Dose 1 (mg)

Dose 2 (mg)

Dose 3 (mg)

Cefixime

50.00

100.00

200.00

Hydrogenated Soy Lecithin

220.00

440.00

880.00

Hydrogenated Egg Yolk Lecithin

220.00

440.00

880.00

cholesterol

440.00

880.00

1760.00

Polysorbate 80

75.00

150.00

300.00

total

1005.00

2010.00

4020.00

[0072] Preparation:

[0073] (A) Dissolve hydrogenated soy lecithin, hydrogenated egg yolk lecithin, cholesterol, and polysorbate 80 in an appropriate amount of absolute ethanol according to the prescribed amount, and mix well to obtain solution I; the amount of absolute ethanol used is the amount of cefixime 30 times;

[0074] (B) Weigh the prescribed amount of cefixime, add an appropriate amount of phosphate buffer with a pH of 6.9 to completely dissolve it to obtain a cefixime solution;

[0075] (C) Weigh povidone K according to the prescription amount 30 , Add the above-mentioned phosphate buffer to dis...

Embodiment 2

[0081] Example 2: Preparation of Cefixime Liposome

[0082] Name of raw materials

Dose 1 (mg)

Dose 2 (mg)

Dose 3 (mg)

Cefixime

50.00

100.00

200.00

Hydrogenated Soy Lecithin

175.00

350.00

710.00

Hydrogenated Egg Yolk Lecithin

175.00

350.00

710.00

cholesterol

350.00

710.00

1420.00

Polysorbate 80

60.00

120.00

240.00

total

810.00

1620.00

3240.00

[0083] Preparation:

[0084] (A) Dissolve hydrogenated soy lecithin, hydrogenated egg yolk lecithin, cholesterol, and polysorbate 80 in an appropriate amount of absolute ethanol according to the prescribed amount, and mix well to obtain solution I; the amount of absolute ethanol used is the amount of cefixime 25 times;

[0085] (B) Weigh the prescribed amount of cefixime and add an appropriate amount of phosphate buffer with a pH of 7.6 to completely dissolve it to obtain a cefixime solution;

[0086] (C) Weigh povidone K according to the prescription amount 30 , Add the above-mentioned phosphate buffer to d...

Embodiment 3

[0092] Example 3: Preparation of Cefixime Liposome

[0093] Name of raw materials

Dose 1 (mg)

Dose 2 (mg)

Dose 3 (mg)

Cefixime

50.00

100.00

200.00

Hydrogenated Soy Lecithin

125.00

250.00

500.00

Hydrogenated Egg Yolk Lecithin

125.00

250.00

500.00

[0094] cholesterol

250.00

500.00

1000.00

Polysorbate 80

42.50

85.00

170.00

total

592.50

1185.00

2370.00

[0095] Preparation:

[0096] (A) Dissolve hydrogenated soy lecithin, hydrogenated egg yolk lecithin, cholesterol, and polysorbate 80 in an appropriate amount of absolute ethanol according to the prescribed amount, and mix well to obtain solution I; the amount of absolute ethanol used is the amount of cefixime 30 times;

[0097] (B) Weigh the prescribed amount of cefixime and add an appropriate amount of phosphate buffer with a pH of 7.8 to completely dissolve it to obtain a cefixime solution;

[0098] (C) Weigh povidone K according to the prescription amount 30 , Add the above-mentioned phosphate ...

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Abstract

The invention relates to a cefixime liposome, a preparation method and a granular formulation containing the cefixime liposome. The granular formulation comprises the cefixime liposome and a pharmaceutically acceptable vector, wherein the cefixime liposome is prepared from the following components in parts by weight: 1 part of cefixime, 1.25-5 parts of hydrogenated soybean lecithin, 1.25-5 parts of hydrogenated egg yolk lecithin, 2.5-10 parts of cholesterol and 0.1-4.5 parts of polysorbate 80. The granular formulation not only accords with the requirement on Chinese pharmacopoeia, but also has the advantages of stabler storage and rapider drug effect exertion and remarkably improved bioavailability compared with the common pharmaceutical cefixime composition at a room temperature.

Description

Technical field [0001] The invention relates to a cefixime liposome, its preparation method and granules containing it. The cefixime granules are more stable in storage and more effective than ordinary cefixime pharmaceutical compositions at room temperature. The advantages of fast speed and significantly improved bioavailability belong to the field of medical technology. Background technique [0002] Acute pelvic inflammatory disease refers to the acute inflammation of female pelvic reproductive organs and surrounding connective tissue, pelvic peritoneum, including metritis, tubal oophoritis, pelvic connective tissue inflammation, and pelvic peritonitis. It can occur in one or several places at the same time. It is a woman One of the common diseases. The development of acute pelvic inflammatory disease can cause diffuse peritonitis, sepsis, septic shock, and severe cases can be life-threatening. Abdominal pain accompanied by fever at the time of onset. If the condition is seve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/34A61P15/00A61P31/00A61K31/546A61K9/16A61K47/26A61K47/28
Inventor 王丽燕
Owner 王丽燕
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